Quinethazone

Names

[ CAS No. ]:
73-49-4

[ Name ]:
Quinethazone

[Synonym ]:
Quimethazin
Quinethazonum
Hydromox
Quinetazona
Quinethazon
Chinethazonum
7-Chlor-6-sulfamoyl-2-aethyl-4-oxo-1,2,3,4-tetrahydro-chinazolin
UNII:455E0S048W
6-Quinazolinesulfonamide, 7-chloro-2-ethyl-1,2,3,4-tetrahydro-4-oxo-
7-Chlor-2-aethyl-6-sulfamoyl-1,2,3,4-tetrahydro-4-chinazolinon
quinethazone
7-chloro-2-ethyl-4-oxo-1,2,3,4-tetrahydro-quinazoline-6-sulfonic acid amide
7-chloro-2-ethyl-1,2,3,4-tetrahydro-4-oxo-6-quinazolinesulfonamide
Aquamox
7-Chloro-2-ethyl-4-oxo-1,2,3,4-tetrahydro-6-quinazolinesulfonamide
7-Chloro-2-ethyl-4-oxo-1,2,3,4-tetrahydroquinazoline-6-sulfonamide
Idrokin

Biological Activity

[Description]:

Quinethazone is an orally active diuretic agent and is also a weak inhibitor of carbonic anhydrase. Quinethazone can be used for hypertension research[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase

[In Vivo]

Quinethazone (50 mg/kg; p.o.; daily for 2 weeks) lowers blood pressure of renal hypertensive rats in association with a decrease in potassium but no change in water or sodium contents of aorta wall[1]. Animal Model: Five- to 6-week-old Long Evans male rats, hypertension model[1] Dosage: 50 mg/kg Administration: Oral, daily for 2 weeks Result: Had no significant effect on sodium or water distribution in arterial tissue of hypertensive rats, but decreased approximate 20% intra-cellular content of potassium

[References]

[1]. FREED SC. MECHANISM OF ANTI-HYPERTENSIVE ACTION OF QUINETHAZONE. Proc Soc Exp Biol Med. 1963 Nov;114:421-2.

[2]. Angelopoulos B, et al. Experimental investigation and observations on the diuretic action of quinethazone. Med Pharmacol Exp Int J Exp Med. 1966;14(6):528-36.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Melting Point ]:
250 - 252ºC

[ Molecular Formula ]:
C₁₀H₁₂ClN₃O₃S

[ Molecular Weight ]:
289.739

[ Exact Mass ]:
289.028778

[ PSA ]:
109.67000

[ LogP ]:
0.49

[ Index of Refraction ]:
1.582

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VA1679500

CHEMICAL NAME :: 6-Quinazolinesulfonamide, 1,2,3,4-tetrahydro-7-chloro-2-ethyl-4-oxo-

CAS REGISTRY NUMBER :: 73-49-4

BEILSTEIN REFERENCE NO. :: 0818554

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C10-H12-Cl-N3-O3-S

MOLECULAR WEIGHT :: 289.76

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,201,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5486 No. of Facilities: 16 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 94 (estimated) No. of Female Employees: 62 (estimated)

Safety Information

[ RIDADR ]:
NONH for all modes of transport